WO2009009042A1 - Methods for synthesizing substituted tetracycline compounds - Google Patents

Methods for synthesizing substituted tetracycline compounds Download PDF

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Publication number
WO2009009042A1
WO2009009042A1 PCT/US2008/008355 US2008008355W WO2009009042A1 WO 2009009042 A1 WO2009009042 A1 WO 2009009042A1 US 2008008355 W US2008008355 W US 2008008355W WO 2009009042 A1 WO2009009042 A1 WO 2009009042A1
Authority
WO
WIPO (PCT)
Prior art keywords
substituted
tetracycline
compound
carboxaldehyde
minocycline
Prior art date
Application number
PCT/US2008/008355
Other languages
English (en)
French (fr)
Inventor
Farzaneh Seyedi
Tadeusz Warchol
Mark Grier
Original Assignee
Paratek Pharmaceuticals, Inc.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority to JP2010514886A priority Critical patent/JP2010532759A/ja
Priority to AU2008275701A priority patent/AU2008275701B2/en
Application filed by Paratek Pharmaceuticals, Inc. filed Critical Paratek Pharmaceuticals, Inc.
Priority to DK08826197.9T priority patent/DK2176216T3/da
Priority to CA2693376A priority patent/CA2693376A1/en
Priority to CN200880105304A priority patent/CN101784517A/zh
Priority to ES08826197T priority patent/ES2386926T3/es
Priority to EP08826197A priority patent/EP2176216B1/de
Priority to BRPI0813990-3A priority patent/BRPI0813990A2/pt
Priority to EA201070048A priority patent/EA201070048A1/ru
Priority to AT08826197T priority patent/ATE555079T1/de
Publication of WO2009009042A1 publication Critical patent/WO2009009042A1/en
Priority to ZA2010/00034A priority patent/ZA201000034B/en
Priority to IL204133A priority patent/IL204133A0/en
Priority to AU2010200845A priority patent/AU2010200845B2/en
Priority to HK10106266.2A priority patent/HK1139386A1/xx
Priority to HRP20120605AT priority patent/HRP20120605T1/hr

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C231/00—Preparation of carboxylic acid amides
    • C07C231/12—Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00—Systems containing at least three condensed rings
    • C07C2603/02—Ortho- or ortho- and peri-condensed systems
    • C07C2603/40—Ortho- or ortho- and peri-condensed systems containing four condensed rings
    • C07C2603/42—Ortho- or ortho- and peri-condensed systems containing four condensed rings containing only six-membered rings
    • C07C2603/44—Naphthacenes; Hydrogenated naphthacenes

Definitions

  • the palladium catalyst is PdCl 2 CtBu 2 PhP) 2 dichlorobis(di-tert- butylphenylphosphine palladium (H)] or PdCl 2 (DPEPhos) [bis(diphenylphosphinophenyl)ether palladium (II) chloride].
  • tetracycline compound includes substituted or unsubstituted tetracycline compounds or compounds with a similar ring structure to tetracycline.
  • tetracycline compounds include: chlortetracycline, oxytetracycline, demeclocycline, methacycline, sancycline, chelocardin, rolitetracycline, lymecycline, apicycline; clomocycline, guamecycline, meglucycline, mepylcycline, minocycline, penimepicycline, pipacycline, etamocycline, penimocycline, etc.
  • the invention pertains to methods for synthesizing a carboxaldehyde substituted tetracycline by reacting a tetracycline reactive intermediate under appropriate conditions.
  • appropriate conditions includes any conditions that are suitable for carrying out the reaction of converting the tetracycline reactive intermediate to the carboxaldehyde substituted tetracycline.
  • Appropriate conditions include any suitable solvents, temperature, catalysts and reagents. A skilled artisan would readily be able to determine appropriate conditions for carrying out the methods of the invention.
  • R 6 and R 6 are each independently hydrogen, methylene, absent, hydroxyl, halogen, thiol, alkyl, alkenyl, alkynyl, aryl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, or an arylalkyl;
  • R 8 is alkyl, alkenyl, alkynyl, aryl, arylalkyl, arylalkenyl or arylalkynyl, formyl or carbonyl;
  • alkenyl further includes alkenyl groups which include oxygen, nitrogen, sulfur or phosphorous atoms replacing one or more carbons of the hydrocarbon backbone.
  • a straight chain or branched chain alkenyl group has 10 or fewer carbon atoms in its backbone (e.g., C 2 -CiO or straight chain, C 3 -C 1O for branched chain).
  • cycloalkenyl groups may have from 3-10 carbon atoms in their ring structure.
  • C 2 -C 1O includes alkenyl groups containing 2 to 10 carbon atoms.
  • substituted alkenyl includes alkenyl moieties having substituents replacing a hydrogen on one or more carbons of the hydrocarbon backbone.

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
PCT/US2008/008355 2007-07-06 2008-07-07 Methods for synthesizing substituted tetracycline compounds WO2009009042A1 (en)

Priority Applications (15)

Application Number Priority Date Filing Date Title
EA201070048A EA201070048A1 (ru) 2007-07-06 2008-07-07 Способы синтеза замещённых соединений тетрациклина (варианты)
BRPI0813990-3A BRPI0813990A2 (pt) 2007-07-06 2008-07-07 métodos para sintetizar compostos de minociclina substituìda
DK08826197.9T DK2176216T3 (da) 2007-07-06 2008-07-07 Fremgangsmåder til syntetisering af 9-substitueret minocyclin
AU2008275701A AU2008275701B2 (en) 2007-07-06 2008-07-07 Methods for synthesizing substituted tetracycline compounds
CN200880105304A CN101784517A (zh) 2007-07-06 2008-07-07 合成取代的四环素化合物的方法
ES08826197T ES2386926T3 (es) 2007-07-06 2008-07-07 Métodos para sintetizar minociclina9-sustituida
AT08826197T ATE555079T1 (de) 2007-07-06 2008-07-07 Verfahren zur synthese von 9-substituiertem minocyclin
JP2010514886A JP2010532759A (ja) 2007-07-06 2008-07-07 置換テトラサイクリン化合物を合成するための方法
CA2693376A CA2693376A1 (en) 2007-07-06 2008-07-07 Methods for synthesizing substituted tetracycline compounds
EP08826197A EP2176216B1 (de) 2007-07-06 2008-07-07 Verfahren zur synthese von 9-substituiertem minocyclin
ZA2010/00034A ZA201000034B (en) 2007-07-06 2010-01-04 Methods for synthesizing substituted tetracycline compounds
IL204133A IL204133A0 (en) 2007-07-06 2010-02-24 Methods for synthesizing substituted tetracycline compounds
AU2010200845A AU2010200845B2 (en) 2007-07-06 2010-03-05 Methods for synthesizing substituted tetracycline compounds
HK10106266.2A HK1139386A1 (en) 2007-07-06 2010-06-25 Methods for synthesizing 9-substituted minocycline 9-
HRP20120605AT HRP20120605T1 (hr) 2007-07-06 2012-07-23 Postupci sinteze 9-supstituiranog minociklina

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US94838507P 2007-07-06 2007-07-06
US60/948,385 2007-07-06
US6035108P 2008-06-10 2008-06-10
US61/060,351 2008-06-10

Publications (1)

Publication Number Publication Date
WO2009009042A1 true WO2009009042A1 (en) 2009-01-15

Family

ID=39926392

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2008/008355 WO2009009042A1 (en) 2007-07-06 2008-07-07 Methods for synthesizing substituted tetracycline compounds

Country Status (18)

Country Link
US (2) US9522872B2 (de)
EP (2) EP2176216B1 (de)
JP (2) JP2010532759A (de)
KR (1) KR20100042276A (de)
CN (2) CN101811980A (de)
AT (1) ATE555079T1 (de)
AU (2) AU2008275701B2 (de)
BR (2) BRPI0823405A2 (de)
CA (1) CA2693376A1 (de)
DK (1) DK2176216T3 (de)
EA (2) EA201070233A1 (de)
ES (1) ES2386926T3 (de)
HK (1) HK1139386A1 (de)
HR (1) HRP20120605T1 (de)
IL (1) IL204133A0 (de)
PT (1) PT2176216E (de)
WO (1) WO2009009042A1 (de)
ZA (2) ZA201000034B (de)

Cited By (3)

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WO2012065028A2 (en) 2010-11-11 2012-05-18 Concert Pharmaceuticals Inc. Substituted tetracyclines
US8946196B2 (en) 2007-04-27 2015-02-03 Paratek Pharmaceuticals, Inc. Methods for synthesizing and purifying aminoalkyl tetracycline compounds
EP3774723A4 (de) * 2018-04-06 2022-03-09 Paratek Pharmaceuticals, Inc. Verfahren zur herstellung von sarecyclin-hydrochlorid

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US7094806B2 (en) 2000-07-07 2006-08-22 Trustees Of Tufts College 7, 8 and 9-substituted tetracycline compounds
US20060287283A1 (en) * 2003-07-09 2006-12-21 Paratek Pharmaceuticals, Inc. Prodrugs of 9-aminomethyl tetracycline compounds
EA201100956A1 (ru) * 2003-07-09 2012-01-30 Пэрэтек Фамэсьютикэлс, Инк. Замещенные соединения тетрациклина (варианты), фармацевтическая композиция и способ лечения чувствительного к тетрациклину состояния у субъекта
EP2284156A3 (de) * 2004-10-25 2011-09-21 Paratek Pharmaceuticals, Inc. Substituierte Tetracyclin-Verbindungen
AU2006210406C1 (en) * 2005-02-04 2013-03-07 Paratek Pharmaceuticals, Inc. 11a, 12-derivatives of tetracycline compounds
CA2616224A1 (en) * 2005-07-21 2007-02-01 Paratek Pharmaceuticals, Inc. 10-substituted tetracyclines and methods of use thereof
WO2007133797A2 (en) * 2006-05-15 2007-11-22 Paratek Pharmaceuticals, Inc. Methods of regulating expression of genes or of gene products using substituted tetracycline compounds
BRPI0720569B8 (pt) * 2006-12-21 2021-05-25 Paratek Pharm Innc compostos de tetraciclina substituída e uso dos ditos compostos para o tratamento de uma infecção bacteriana, viral ou parasitária
AU2007338681B2 (en) 2006-12-21 2013-09-26 Paratek Pharmaceuticals, Inc. Substituted tetracycline compounds for treatment of inflammatory skin disorders
WO2008127722A1 (en) 2007-04-12 2008-10-23 Paratek Pharmaceuticals, Inc. Methods for treating spinal muscular atrophy using tetracycline compounds
EP2262754A4 (de) * 2008-03-05 2012-03-14 Paratek Pharm Innc Minocyclinverbindungen und anwendungsverfahren dafür
EP2276342A4 (de) * 2008-04-14 2012-02-22 Paratek Pharm Innc Substituierte tetracyclinverbindungen
KR20110081197A (ko) * 2008-09-19 2011-07-13 파라테크 파마슈티컬스, 인크. 류마티스 관절염의 치료를 위한 테트라시클린 화합물 및 관련된 치료 방법
WO2011025982A2 (en) * 2009-08-28 2011-03-03 Tetraphase Pharmaceuticals, Inc. Tetracycline compounds
NZ740051A (en) 2012-08-31 2019-09-27 Tetraphase Pharmaceuticals Inc Tetracycline compounds
EP3529236B1 (de) 2016-10-19 2024-02-07 Tetraphase Pharmaceuticals, Inc. Kristalline formen von eravacyclin
SG10201913599RA (en) 2016-11-01 2020-02-27 Paratek Pharm Innc 9-aminomethyl minocycline compounds and use thereof in treating community-acquired bacterial pneumonia (cabp)
PT117254B (pt) 2021-05-26 2024-04-18 Hovione Farm S A Método de síntese de compostos 9-aminometil tetraciclinas

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US8946196B2 (en) 2007-04-27 2015-02-03 Paratek Pharmaceuticals, Inc. Methods for synthesizing and purifying aminoalkyl tetracycline compounds
US9434680B2 (en) 2007-04-27 2016-09-06 Paratek Pharmaceuticals, Inc. Methods for synthesizing and purifying aminoalkyl tetracycline compounds
WO2012065028A2 (en) 2010-11-11 2012-05-18 Concert Pharmaceuticals Inc. Substituted tetracyclines
EP3774723A4 (de) * 2018-04-06 2022-03-09 Paratek Pharmaceuticals, Inc. Verfahren zur herstellung von sarecyclin-hydrochlorid
AU2019248350B2 (en) * 2018-04-06 2023-07-27 Almirall, Llc Process for making sarecycline hydrochloride

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